EP4028403C0 - 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors - Google Patents
4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitorsInfo
- Publication number
- EP4028403C0 EP4028403C0 EP20774901.1A EP20774901A EP4028403C0 EP 4028403 C0 EP4028403 C0 EP 4028403C0 EP 20774901 A EP20774901 A EP 20774901A EP 4028403 C0 EP4028403 C0 EP 4028403C0
- Authority
- EP
- European Patent Office
- Prior art keywords
- hexapyrido
- oxazin
- compounds
- magl inhibitors
- magl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- XEKAWZARUWARND-UHFFFAOYSA-N 6h-oxazin-3-one Chemical class O=C1NOCC=C1 XEKAWZARUWARND-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/485—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Inorganic Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP19196879 | 2019-09-12 | ||
| PCT/EP2020/075260 WO2021048242A1 (en) | 2019-09-12 | 2020-09-10 | 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| EP4028403A1 EP4028403A1 (en) | 2022-07-20 |
| EP4028403B1 EP4028403B1 (en) | 2023-11-22 |
| EP4028403C0 true EP4028403C0 (en) | 2023-11-22 |
Family
ID=67953598
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP20774901.1A Active EP4028403B1 (en) | 2019-09-12 | 2020-09-10 | 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US11814375B2 (en) |
| EP (1) | EP4028403B1 (en) |
| JP (1) | JP2022548028A (en) |
| KR (1) | KR20220062515A (en) |
| CN (1) | CN114269755A (en) |
| AR (1) | AR119943A1 (en) |
| AU (1) | AU2020346350A1 (en) |
| BR (1) | BR112022002375A2 (en) |
| CA (1) | CA3151516A1 (en) |
| CL (1) | CL2022000556A1 (en) |
| CO (1) | CO2022001879A2 (en) |
| CR (1) | CR20220104A (en) |
| IL (1) | IL289186A (en) |
| MX (1) | MX2022002311A (en) |
| PE (1) | PE20220565A1 (en) |
| TW (1) | TW202128706A (en) |
| WO (1) | WO2021048242A1 (en) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10357493B2 (en) | 2017-03-10 | 2019-07-23 | Selenity Therapeutics (Bermuda), Ltd. | Metalloenzyme inhibitor compounds |
| AR114136A1 (en) | 2017-10-10 | 2020-07-29 | Hoffmann La Roche | HETEROCYCLIC COMPOUNDS |
| WO2019105915A1 (en) | 2017-11-28 | 2019-06-06 | F. Hoffmann-La Roche Ag | New heterocyclic compounds |
| TW201938164A (en) | 2018-01-08 | 2019-10-01 | 瑞士商赫孚孟拉羅股份公司 | New heterocyclic compounds |
| PE20211089A1 (en) | 2018-08-13 | 2021-06-14 | Hoffmann La Roche | NEW HETEROCYCLIC COMPOUNDS AS INHIBITORS OF MONACILGLICEROL LIPASE |
| BR112022002375A2 (en) | 2019-09-12 | 2022-07-19 | Hoffmann La Roche | 4,4A,5,7,8,8A-HEXAPYRIDO[4,3-B][1,4]OXAZIN-3-ONA COMPOUNDS AS MAGL INHIBITORS |
| CN114980887A (en) | 2019-12-20 | 2022-08-30 | 特纳亚治疗股份有限公司 | Fluoroalkyl-oxadiazoles and their use |
| MX2023002224A (en) | 2020-09-03 | 2023-03-15 | Hoffmann La Roche | Heterocyclic compounds. |
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| US7160888B2 (en) | 2003-08-22 | 2007-01-09 | Warner Lambert Company Llc | [1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia |
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| ES2337728T3 (en) | 2005-06-20 | 2010-04-28 | Schering Corporation | PIPERIDINES REPLACED TO CARBON AND ITS USEFUL DERIVATIVES AS HISTAMINE ANTAGONISTS H3. |
| JP5116687B2 (en) | 2005-11-02 | 2013-01-09 | バイエル・ファルマ・アクチェンゲゼルシャフト | Pyrrolo [2,1-f] [1,2,4] triazin-4-ylamine IGF-1R kinase inhibitors for the treatment of cancer and other hyperproliferative diseases |
| CA2637531A1 (en) | 2006-02-17 | 2007-08-30 | Memory Pharmaceuticals Corporation | Compounds having 5-ht6 receptor affinity |
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| TW200942537A (en) | 2008-02-01 | 2009-10-16 | Irm Llc | Compounds and compositions as kinase inhibitors |
| WO2010049302A1 (en) | 2008-10-29 | 2010-05-06 | F. Hoffmann-La Roche Ag | Novel phenyl amide or pyridil amide derivatives and their use as gpbar1 agonists |
| WO2011059118A1 (en) | 2009-11-10 | 2011-05-19 | Kim Hyun Jeen | System for testing olfactory perception |
| WO2011058766A1 (en) | 2009-11-16 | 2011-05-19 | Raqualia Pharma Inc. | Aryl carboxamide derivatives as ttx-s blockers |
| US8420661B2 (en) | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
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| WO2013059118A1 (en) | 2011-10-19 | 2013-04-25 | The Trustees Of Columbia University In The City Of New York | Cyclopropenimine catalyst compositions and processes |
| TW201326180A (en) | 2011-11-30 | 2013-07-01 | Actelion Pharmaceuticals Ltd | 3,7-disubstituted octahydro-2H-pyrido[4,3-e][1,3]oxazin-2-one antibiotics |
| PL2794600T3 (en) | 2011-12-22 | 2018-06-29 | Novartis Ag | 2,3-Dihydro-benzo[1,4]oxazine derivatives and related compounds as phosphoinositide-3 kinase (PI3K) inhibitors for the treatment of e.g. rheumatoid arthritis |
| AU2013207252B2 (en) | 2012-01-06 | 2016-06-09 | H.Lundbeck A/S | Carbamate compounds and pharmaceutical compositions thereof |
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| CN111148746B (en) | 2017-09-29 | 2022-08-05 | 武田药品工业株式会社 | Heterocyclic compounds |
| AR114136A1 (en) | 2017-10-10 | 2020-07-29 | Hoffmann La Roche | HETEROCYCLIC COMPOUNDS |
| WO2019105915A1 (en) | 2017-11-28 | 2019-06-06 | F. Hoffmann-La Roche Ag | New heterocyclic compounds |
| TW201930300A (en) | 2017-12-15 | 2019-08-01 | 瑞士商赫孚孟拉羅股份公司 | New heterocyclic compounds |
| TW201938164A (en) | 2018-01-08 | 2019-10-01 | 瑞士商赫孚孟拉羅股份公司 | New heterocyclic compounds |
| SI3768684T1 (en) | 2018-03-22 | 2023-06-30 | F. Hoffmann - La Roche Ag | Oxazine monoacylglycerol lipase (magl) inhibitors |
| PE20211089A1 (en) | 2018-08-13 | 2021-06-14 | Hoffmann La Roche | NEW HETEROCYCLIC COMPOUNDS AS INHIBITORS OF MONACILGLICEROL LIPASE |
| PE20211380A1 (en) | 2018-08-13 | 2021-07-27 | Hoffmann La Roche | NEW HETEROCYCLIC COMPOUNDS AS MONOACYLGLICEROL LIPASE INHIBITORS |
| PL3883936T3 (en) | 2018-11-22 | 2023-11-20 | F. Hoffmann-La Roche Ag | New heterocyclic compounds |
| US20220024901A1 (en) | 2018-11-22 | 2022-01-27 | Qilu Regor Therapeutics Inc. | Glp-1r agonists and uses thereof |
| EP3953360B1 (en) | 2019-04-09 | 2024-02-28 | F. Hoffmann-La Roche AG | Heterocyclic compounds as inhibitors of monoacylglycerol lipase (magl) |
| PE20220514A1 (en) | 2019-07-03 | 2022-04-07 | Hoffmann La Roche | HETEROCYCLIC MONOACYLGLYCEROL LIPASE (MAGL) INHIBITORS |
| CA3145338A1 (en) | 2019-07-09 | 2021-01-14 | F. Hoffmann-La Roche Ag | New heterocyclic compounds |
| US20210094971A1 (en) | 2019-09-09 | 2021-04-01 | Hoffmann-La Roche Inc. | Heterocyclic compounds |
| WO2021048241A1 (en) | 2019-09-12 | 2021-03-18 | F. Hoffmann-La Roche Ag | Radiolabeled compounds |
| BR112022002375A2 (en) | 2019-09-12 | 2022-07-19 | Hoffmann La Roche | 4,4A,5,7,8,8A-HEXAPYRIDO[4,3-B][1,4]OXAZIN-3-ONA COMPOUNDS AS MAGL INHIBITORS |
| JP2022549810A (en) | 2019-09-23 | 2022-11-29 | エフ．ホフマン－ラ ロシュ アーゲー | heterocyclic compound |
| BR112022003357A2 (en) * | 2019-09-24 | 2022-05-17 | Hoffmann La Roche | Heterocyclic compounds |
| EP4034602A1 (en) | 2019-09-24 | 2022-08-03 | F. Hoffmann-La Roche AG | Fluorescent probes for monoacylglycerol lipase (magl) |
| WO2021058445A1 (en) | 2019-09-24 | 2021-04-01 | F. Hoffmann-La Roche Ag | New heterocyclic monoacylglycerol lipase (magl) inhibitors |
| MX2023002224A (en) | 2020-09-03 | 2023-03-15 | Hoffmann La Roche | Heterocyclic compounds. |
-
2020
- 2020-09-10 BR BR112022002375A patent/BR112022002375A2/en unknown
- 2020-09-10 AU AU2020346350A patent/AU2020346350A1/en active Pending
- 2020-09-10 JP JP2022516054A patent/JP2022548028A/en active Pending
- 2020-09-10 CA CA3151516A patent/CA3151516A1/en active Pending
- 2020-09-10 EP EP20774901.1A patent/EP4028403B1/en active Active
- 2020-09-10 MX MX2022002311A patent/MX2022002311A/en unknown
- 2020-09-10 CN CN202080059190.8A patent/CN114269755A/en active Pending
- 2020-09-10 CR CR20220104A patent/CR20220104A/en unknown
- 2020-09-10 PE PE2022000245A patent/PE20220565A1/en unknown
- 2020-09-10 WO PCT/EP2020/075260 patent/WO2021048242A1/en unknown
- 2020-09-10 US US17/017,200 patent/US11814375B2/en active Active
- 2020-09-10 KR KR1020227007925A patent/KR20220062515A/en unknown
- 2020-09-11 AR ARP200102527A patent/AR119943A1/en unknown
- 2020-09-11 TW TW109131236A patent/TW202128706A/en unknown
-
2021
- 2021-12-20 IL IL289186A patent/IL289186A/en unknown
-
2022
- 2022-02-22 CO CONC2022/0001879A patent/CO2022001879A2/en unknown
- 2022-03-07 CL CL2022000556A patent/CL2022000556A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL289186A (en) | 2022-02-01 |
| CA3151516A1 (en) | 2021-03-18 |
| JP2022548028A (en) | 2022-11-16 |
| AR119943A1 (en) | 2022-01-19 |
| BR112022002375A2 (en) | 2022-07-19 |
| US20210094943A1 (en) | 2021-04-01 |
| EP4028403B1 (en) | 2023-11-22 |
| US11814375B2 (en) | 2023-11-14 |
| KR20220062515A (en) | 2022-05-17 |
| CO2022001879A2 (en) | 2022-03-29 |
| EP4028403A1 (en) | 2022-07-20 |
| CN114269755A (en) | 2022-04-01 |
| CR20220104A (en) | 2022-04-20 |
| TW202128706A (en) | 2021-08-01 |
| PE20220565A1 (en) | 2022-04-13 |
| WO2021048242A1 (en) | 2021-03-18 |
| AU2020346350A1 (en) | 2022-02-17 |
| CL2022000556A1 (en) | 2022-10-21 |
| MX2022002311A (en) | 2022-03-25 |
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